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Compound Detail

CHEMBL1933279

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Cn1c(NC(=O)c2ccc3cc4n(c3c2)CCCNC4=O)nc2ccccc21

Basic Information

ChEMBL ID CHEMBL1933279
Phase Preclinical
Structure Type MOL
InChI Key WIICYVHPNFINMO-UHFFFAOYSA-N
2
Targets
5
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

373.4
MW (Da)
2.91
ALogP
5
HBA
2
HBD
81.0
PSA (Ų)
0.57
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H19N5O2
MW 373.42
Aromatic Rings 4
Heavy Atoms 28
NP-Likeness -1.02

Activity Summary

IC50 5 meas. best 8.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Ribosomal protein S6 kinase alpha-3
CHEMBL2345
IC50 8.05 7.375 9.0 4
Ribosomal protein S6 kinase alpha-2
CHEMBL3906
IC50 8.05 8.05 9.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
22056746 10.1016/j.bmcl.2011.10.029 Ribosomal protein S6 kinase alpha-3 2
22100312 10.1016/j.bmcl.2011.10.030 Ribosomal protein S6 kinase alpha-3 2
22056746 10.1016/j.bmcl.2011.10.029 MAP kinase-activated protein kinase 5 1
22056746 10.1016/j.bmcl.2011.10.029 Cyclin-dependent kinase 1/cyclin B1 1
22056746 10.1016/j.bmcl.2011.10.029 Aurora kinase B 1
22056746 10.1016/j.bmcl.2011.10.029 Aurora kinase A 1
22056746 10.1016/j.bmcl.2011.10.029 AMP-activated protein kinase (AMPK) alpha-1/beta-1/gamma-1 1
22056746 10.1016/j.bmcl.2011.10.029 Proto-oncogene tyrosine-protein kinase receptor Ret 1
22056746 10.1016/j.bmcl.2011.10.029 Serine/threonine-protein kinase D1 1
22056746 10.1016/j.bmcl.2011.10.029 Platelet-derived growth factor receptor alpha 1
22056746 10.1016/j.bmcl.2011.10.029 High affinity nerve growth factor receptor 1
22056746 10.1016/j.bmcl.2011.10.029 Serine/threonine-protein kinase Chk2 1
22056746 10.1016/j.bmcl.2011.10.029 Mitogen-activated protein kinase kinase kinase kinase 4 1
22056746 10.1016/j.bmcl.2011.10.029 Mitogen-activated protein kinase kinase kinase kinase 2 1
22056746 10.1016/j.bmcl.2011.10.029 Dual specificity mitogen-activated protein kinase kinase 1 1
22056746 10.1016/j.bmcl.2011.10.029 Leucine-rich repeat serine/threonine-protein kinase 2 1
22056746 10.1016/j.bmcl.2011.10.029 Vascular endothelial growth factor receptor 2 1
22056746 10.1016/j.bmcl.2011.10.029 Fibroblast growth factor receptor 2 1
22056746 10.1016/j.bmcl.2011.10.029 Dual specificity tyrosine-phosphorylation-regulated kinase 1A 1
22056746 10.1016/j.bmcl.2011.10.029 Dual specificity protein kinase CLK2 1

Data from ChEMBL 36 via Core Engine